A series of new benzofuran‐1,3,4‐oxadiazole containing 1,2,3‐triazole‐acetamides 12a‐n as potential anti‐α‐glucosidase agents were designed and synthesized. α‐Glucosidase inhibition assay demonstrated that all the synthesized compounds 12a‐n (half‐maximal inhibitory concentration [IC₅₀] values in the range of 40.7 ± 0.3–173.6 ± 1.9 μM) were more potent than standard inhibitor acarbose (IC₅₀ = 750.0 ± 12.5 µM). Among them, the most potent compound was compound 12c, with inhibitory activity around 19‐fold higher than acarbose. Since the most potent compound inhibited α‐glucosidase in a competitive mode, a docking study of this compound was also performed into the active site of α‐glucosidase. In vitro and in silico toxicity assays of the title compounds were also performed.

中文翻译：

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含有1,2,3-三唑-乙酰胺作为潜在的α-葡萄糖苷酶抑制剂的一系列新的苯并呋喃-1,3,4-恶二唑的合成和生物学评估

设计并合成了一系列新的苯并呋喃-1,3,4-恶二唑，其中含有1,2,3-三唑-乙酰胺12a-n作为潜在的抗α-葡萄糖苷酶试剂。α-葡萄糖苷酶抑制试验表明，所有合成的化合物12a-n（半数最大抑制浓度[IC ₅₀ ]值在40.7±0.3–173.6±1.9μM范围内）均比标准抑制剂阿卡波糖（IC ₅₀  = 750.0 ）更有效±12.5 µM）。其中，最有效的化合物是化合物12c，其抑制活性比阿卡波糖高约19倍。由于最有效的化合物以竞争性方式抑制α-葡萄糖苷酶，因此该化合物的对接研究也进入了α-葡萄糖苷酶的活性位点。还进行了标题化合物的体外和计算机毒性分析。